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Title: | Synthesis, Characterization, and in vitro Antimalarial and Antitumor Activity of New Ruthenium(II) Complexes of Chloroquine |
Authors: | Rajapakse, C.S.K. Martínez, A. Naoulou, B. Jarzecki, A.A. Suárez, L. Deregnaucourt, C. Sinou, V. Schrével, J. Musi, E. Ambrosini, G. Schwartz, G.K. Sánchez-Delgado, R.A. |
Issue Date: | 2009 |
Publisher: | Journal of Inorganic Chemistry |
Abstract: | The new RuII chloroquine complexes [Ru(?6-arene)(CQ)Cl2] (CQ = chloroquine; arene = p-cymene 1, benzene 2), [Ru(?6-p-cymene)(CQ)(H2O)2][BF4]2 (3), [Ru(?6-p-cymene)(CQ)(en)][PF6]2 (en = ethylenediamine) (4), and [Ru(?6-p-cymene)(?6-CQDP)][BF4]2 (5, CQDP = chloroquine diphosphate) have been synthesized and characterized by use of a combination of NMR and FTIR spectroscopy with DFT calculations. Each complex is formed as a single coordination isomer: In 1?4, chloroquine binds to ruthenium in the ?1-N mode through the quinoline nitrogen atom, whereas in 5 an unprecedented ?6 bonding through the carbocyclic ring is observed. 1, 2, 3, and 5 are active against CQ-resistant (Dd2, K1, and W2) and CQ-sensitive (FcB1, PFB, F32, and 3D7) malaria parasites (Plasmodium falciparum); importantly, the potency of these complexes against resistant parasites is consistently higher than that of the standard drug chloroquine diphosphate. 1 and 5 also inhibit the growth of colon cancer cells, independently of the p53 status and of liposarcoma tumor cell lines with the latter showing increased sensitivity, especially to 1 (IC50 8 ?M); this is significant because this type of tumor does not respond to currently employed chemotherapies |
URI: | http://repository.kln.ac.lk/handle/123456789/3883 |
ISSN: | 0020-1669 (print), 1520-510X (web) |
Appears in Collections: | Chemistry |
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